psychologywikiaorg-20200213-history
Nabilone
| CAS_number = 51022-71-0 | ATC_prefix = A04 | ATC_suffix = AD11 | ATC_supplemental = | PubChem = 5284592 | DrugBank = APRD01127 | C=24 | H=36 | O=3 | molecular_weight = 372.541 g/mol | bioavailability = 20% after first-pass by the liver | protein_bound = similar to THC (+/-97%) | T-max = 2 hours | duration of action = 8-12 hours | onset of action = 60-90 minutes | THC equivalence = 1mg = 10mg THC | metabolism = | Number of metabolite = 2 actives metabolites | Excretion = Feces(65%)and urine(20%) | elimination_half-life = 2 hours, with metabolites around 35 hours. | Marijuana Drug test (EMIT) = negative | pregnancy_category = NA | legal_US = Schedule II | routes_of_administration = Oral form (PO)- capsule | Availability = 0.5 mg and 1 mg capsule }} Nabilone is a synthetic cannabinoid with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It is a synthetic cannabinoid, which mimics the main ingredient of marijuana (THC). Chemically, nabilone is similar to the active ingredient found in naturally occurring Cannabis sativa L. Nabilone is not listed as a narcotic by WHO as it lacks the euphoric and recreational potential of other cannabinoids. In Canada, the United States, the United Kingdom and Mexico, nabilone is marketed as Cesamet. It was approved in 1985 by the U.S. Food and Drug Administration (FDA) for treatment of chemotherapy-induced nausea and vomiting that has not responded to conventional antiemetics. Though it was approved by the FDA in 1985, the drug only began marketing in the United States in 2006. It is also approved for use in treatment of anorexia and weight loss in patients with AIDS. Although it doesn't have the official indication (except in Mexico), nabilone is widely used as an adjunct therapy for chronic pain management. Numerous trials and case studies have demonstrated various benefits for condition such as fibromyalgia and multiple sclerosis. Nabilone is a racemic mixture consisting of the (S,S) and the (R,R) isomers ("trans"). Clinical trials The main settings that have seen published clinical trials of nabilone include movement disorders such as Parkinson's syndrome, chronic pain, dystonia and spasticity neurological disorders, fibromyalgia, multiple sclerosis, and the nausea of cancer chemotherapy. A study comparing nabilone with metoclopramide, conducted before the development of modern 5-HT3 inhibitor anti-emetics such as ondansetron, revealed that patients taking cisplatin chemotherapy preferred metoclopramide, while patients taking carboplatin chemotherapy preferred nabilone to control nausea and vomiting. Another study compared nabilone alone to nabilone with dexamethasone. The study found that the combination worked better than the single medication. An older study revealed that nabilone was more effective than prochlorperazine in controlling nausea, though in this study, only 9% of nabilone patients had complete resolution of symptoms. A follow-up to this study revealed similar findings. One study compared the efficacy and tolerability of nabilone with that of dihydrocodeine in the treatment of neuropathic pain.Frank B, Serpell MG, Hughes J, Matthews JN, Kapur D. "Comparison of analgesic effects and patient tolerability of nabilone and dihydrocodeine for chronic neuropathic pain: randomised, crossover, double blind study." British Medical Journal. 2008 Jan 8. ahead of print. PMID 18182416. The authors found that nabilone was not as effective as dihydrocodeine in controlling pain, and caused a higher incidence of minor adverse drug reactions than did dihydrocodeine. One critic of the study has suggested that nabilone might be best suited for the treatment of patients suffering from central and spasticity-related pain, for which there is stronger evidence for the benefits of cannabinoid therapy; however, these patients made up only a small fraction of the study's population, and the study was not designed to identify subgroups which might have responded more favorably to treatment than others.Cohen SP. "Cannabinoids for chronic pain." British Medical Journal. 2008 Jan 8. ahead of print. PMID 18182415. A clinical trial performed in Canada reviewed the use of nabilone to treat nightmares in individuals suffering from post-traumatic stress syndrome . The study found that nighttime administration of nabilone reduced the frequency and/or intensity of nightmares in 34 out of 47 (72%) of patients, with 28 reporting complete cessation of nightmares. This study is limited to the extent that there was no placebo control, but warrants future investigation into the use of cannabinoid therapy in the treatment of post-traumatic stress syndrome and other disorders involving recurrent nightmares. References Category:Cannabinoids